Extraction optimisation,antioxidant activity and inhibition on α-amylase and pancreatic lipase of polyphenols from the seeds of Syzygium cumini

The objectives of this study were to determine the optimal extraction conditions of polyphenols from Syzygium cumini seeds by response surface methodology and investigate their antioxidant activity and inhibition on α-amylase and pancreatic lipase. As results, the optimal extraction conditions in the ultrasonic extraction process which maximised total polyphenols content, minimised the IC₅₀ values of α-amylase and pancreatic lipase were determined as follows: extraction time 60 min, ethanol concentration 63% and solvent/solid ratio 44 mL g⁻¹. The main phenolic compounds in partially purified fraction of Syzygium cumini seeds were catechin, epicatechin, kaempferol, gallic, 5-caffeoylquinic, caffeic and ferulic acids. In addition, the partially purified fraction inhibited 87.66 ± 5.55 and 86.61 ± 3.15% of α-amylase and pancreatic lipase, respectively. The results suggested that Syzygium cumini seeds could be explored as a natural antioxidant and could be used as a source of highly antidiabetic and anti-obesity bioactive compounds.     

Process Optimization,Physical Properties,and Environmental Stability of an α-Tocopherol Nanocapsule Preparation Using Complex Coacervation Method and Full Factorial Design

α-Tocopherol (α-Toc) has valuable biological activity, but its activity is limited when exposed to environmental factors. Nanocapsules can be used to overcome this problem. Using nanocapsules in the range of 100–200 nm is more beneficial. A 2⁴ full factorial design was carried out to optimize the size of nanocapsules using the complex coacervation method. The four factors were the amount of the wall material, the ratio of core material to wall material, the pH of the solution, and the speed of the homogenizer. The smallest nanocapsules (176 nm) were obtained at a wall content (gelatine and pectin) of 0.8 mg, a percentage of core material (α-Toc) to wall material of 20%, a pH = 4.5, and a homogenizer speed of 12,000 rpm. The encapsulation efficiency was 90.6 ± 1.1%, and the encapsulation yield was 83.4 ± 1.6%. Assessment of the stability of α-Toc after 1 month showed that encapsulation could improve its stability in the presence of three influential factors: humidity, light, and temperature.     

Inhibition of proteases activity in intestine needs a sustainable acidic environment rather than a transient

α-Chymotrypsin (α-CT) and trypsin are important components of the enzymatic barrier. They could degrade the therapeutic proteins and peptides, inhibit their activity consequently, and thereby reduce their oral bioavailability. Acidic agents, as one type of indirect protease inhibitors, have shown proof of concept in clinical trials. We report here the inactivated proteases due to acid influence can be reactivated immediately by environmental pH recovery regardless of how long the inactivation last. To keep the inactivation time of proteases for 4–5?h, we designed and prepared a sustained-release tablet containing citric acid (CA) which can effectively reduce the pH below 5.0 and maintain it for 5?h in the dissolution-reaction medium. The activity of α-CT and trypsin was quantified by analyzing the residual amount of their respective substrates BTEE and TAME. More than 80% of the substrates were survived in 5.0?h of incubation, whereas the common tablet inhibited the proteases activity for only two hours in the same experimental medium. It indicates that the sustained-release tablet loaded with CA can efficiently inhibit the α-CT and trypsin activity longer than the common tablet. The results will be beneficial for designing and formulating the peroral administration of peptide and protein drugs.     

Selenium dioxide reaction of substituted diphenacyl sulfides: generation of α -ketoacids

The attempted selenium dioxide oxidation of substituted diphenacyl sulfides in anticipation of further functionalization led to a series of α -ketoacids 3 via oxidation followed by C?S bond cleavage. Two minor products, 5 and 6, have also been isolated and a mechanistic pathway for the formation of 3, 5 and 6 has been proposed.     

Preparation of luminescent layered zirconium phosphate nanocomposites by the layer-by-layer technique

In the present work, photoactive cation N, N′-Dimenthyl-9, 9’-bisacridinium nitrate (BNMA) was assembled with exfoliated layered α-zirconium phosphate (α-ZrP) via an electrostatic layer-by-layer (LBL) assembly method. As a result, the luminescent films which were well-aligned and periodical had been successfully fabricated. Surprisingly, the lifetimes of (BNMA/ZrP)_n were found to be prolonged by 16-fold for the first time, due to the isolation effect of inorganic nanosheets and hydrogen ion migration between the interlayers. Therefore, it is testified that α-ZrP can be used as the laminate and has remarkable influences on enhancing the lifetimes of chromophores. We expect that this new discovered effect can enable α-ZrP a kind of new potential material to develop novel light-emitting materials and optical devices.     

狼毒多糖对TNF-α诱导的内皮细胞P-selectin表达的影响

目的:探讨狼毒多糖(EFP-AW1)对TNF-α诱导的内皮细胞P-selectin表达的影响。方法:以TNF-α诱导HUVECs建立内皮细胞分泌P-selectin模型,流式细胞术检测EFP-AW1对TNF-α诱导的HUVECs细胞P-selectin蛋白表达的影响;Real-time PCR检测EFP-AW1对TNF-α诱导的HUVECs细胞P-selectin m RNA表达的影响。结果:HUVECs经TNF-α刺激后P-selectin表达较空白对照组明显增强(P<0.05),而经过EFP-AW1预处理的HUVECs P-selectin m RNA和蛋白表达水平与TNF-α刺激组比较明显降低(P<0.05),并具有一定的剂量依赖性。结论:EFP-AW1能够降低TNF-α诱导的内皮细胞黏附分子P-selectin表达,从而抑制P-selectin介导的肿瘤细胞与内皮细胞的黏附。     

Potential risk indicators of retained placenta and other diseases in multiparous cows

Retained placenta (RP), defined as fetal membranes not being expelled within 24 h after calving, is a costly disease in multiparous dairy cows that has been linked to immune suppression, infections, elevated lipid mobilization, and depleted status of antioxidants including α-tocopherol, and that increases the risk of other diseases (OD) in early lactation. Early detection of cows at increased risk of developing RP, OD, or both in early lactation could improve treatment success and result in improved milk production and reproductive performance. To identify risk indicators of RP, OD, or both, we used a nested case-control design and compared multiparous dairy cows that developed RP (n = 32) with cows that remained healthy (H; n = 32) or cows that developed OD (n = 32) in early lactation. We compared peripartal body condition score (BCS) as well as serum concentrations of α-tocopherol, metabolites [β-hydroxybutyrate (BHBA), cholesterol, glucose, nonesterified fatty acids (NEFA), and urea N], haptoglobin, and macrominerals (i.e., calcium, magnesium, and phosphorus) on d −21, −14, −7, −3, −1, 0, 1, 3, 7, 14, 21, 28, 35, 42, and 49 postpartum. In addition, average serum concentrations were calculated for each cow for the last 3 wk prepartum, for 3 and 2 wk prepartum combined, for the last week prepartum, and for the morning after calving and compared between groups. The RP cows had lower BCS than the H or OD cows until 2 wk postpartum. During the prepartal periods, RP and OD cows had lower α-tocopherol concentrations (corrected or not for cholesterol concentration) and higher NEFA and BHBA concentrations than H cows. Thus, lower prepartal BCS could be an early predictor for RP risk, and lower α-tocopherol concentrations and higher NEFA and BHBA concentrations could be early predictors for disease.     

微小RNA调控干扰素-α在系统性红斑狼疮发病机制中的作用

系统性红斑狼疮是一种多系统受累的自身免疫病。干扰素-α作为系统性红斑狼疮免疫紊乱的关键因素,对其作用机制及信号通路的研究可进一步揭示系统性红斑狼疮的发病机制,并为该病的临床治疗提供新策略。近年研究发现,微小RNA在系统性红斑狼疮发病机制中具有重要作用,且微小RNA异常表达参与Ⅰ型干扰素通路的调节。本文综述了微小RNA对Ⅰ型干扰素通路的调节及其在系统性红斑狼疮发病机制中的作用,对进一步认识系统性红斑狼疮的发病机制具有重要意义。     

The methionine precursor dl-2-hydroxy-(4-methylthio)butanoic acid protects intestinal epithelial barrier function

dl-2-hydroxy-(4-methylthio)butanoic acid (HMTBA) is a source of dietary methionine (Met) that is widely used in poultry nutrition. We have previously shown that HMTBA is preferentially diverted to the transsulfuration pathway, which gives antioxidant metabolites such as taurine and glutathione. Therefore, here we hypothesize that this Met source can protect epithelial barrier function in an in vitro model of intestinal inflammation of Caco-2 cells. The results show that HMTBA prevents the increase in paracellular permeability induced by H₂O₂ or tumour necrosis factor-α. This effect can be attributed to the increased production of taurine and reduced glutathione. Similar results were obtained for dl-Met, although the protective role of the amino acid was less pronounced than that of the hydroxy analogue. In conclusion, the diversion to the transsulfuration pathway means that this Met precursor is of greater value than previously thought, due to its capacity to improve intestinal homeostasis and the quality of poultry products destined for human consumption.     

3,4-Dimethyl-2,5-functionalized thieno[2,3-b]thiophenes: versatile precursors for novel bis-thiazoles

Synthesis of novel bis(thiazoles) 19–22, 24, 25, 30 and 31 is reported. Thus, reaction of the bis(α-bromoketones) 14 and 15 with the corresponding thioamide derivatives 16–18 in refluxing EtOH in the presence of triethylamine afforded 19–22 in good yields. On the other hand, the novel bis(thiazoles) 24 and 25 can be synthesized by the reaction of 14 and 15 with the corresponding p-chlorobenzaldehyde thiosemicarbazones 23 in refluxing EtOH. The novel isomeric bis(thiazoles) 30 and 31 can also be synthesized by a reaction of the corresponding bis(benzaldehyde thiosemicarbazones) 27 and 28 with p-chlorophenacyl bromide 29. Compounds 27 and 28 were obtained by condensation of the corresponding bis(aldehydes) 12 and 13 with thiosemicarbazide 26.